| DC48226 |
ONO-8430506
Featured
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ONO-8430506 is an orally bioavailable and potent autotaxin (ATX)/ENPP2 inhibitor with the IC90 of 100 nM for ATX activity in mouse plasma. |
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| DC48693 |
Enpp-1-IN-9 |
Enpp-1-IN-9 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-9 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51). |
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| DC48696 |
Enpp-1-IN-5 |
Enpp-1-IN-5 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-5 has the potential for the research of cancer and infectious diseases (extracted from patent WO2019046778A1/WO2021203772A1, compound 1). |
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| DC48714 |
Enpp-1-IN-7 |
Enpp-1-IN-7 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-7 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51). |
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| DC48745 |
Enpp-1-IN-4 |
Enpp-1-IN-4 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). Enpp-1-IN-4 has the potential for the research of cancer diseases (extracted from patent WO2019177971A1, compound 1). |
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| DC48763 |
Enpp-1-IN-8 |
Enpp-1-IN-8 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-8 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51). |
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| DC48871 |
Enpp-1-IN-6 |
Enpp-1-IN-6 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-6 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51). |
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| DC48927 |
Hcyb1 |
Hcyb1 is a highly selective PDE2 inhibitor. Hcyb1 has a highly selective inhibition of PDE2A (IC50=0.57 μM) and over 250-fold selectivity against other recombinant PDE family members. Hcyb1 produces neuroprotective and antidepressant‐like effects most likely mediated by cAMP/cGMP-CREB-BDNF signaling. |
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| DC48957 |
Drotaverine hydrochloride |
Drotaverine (hydrochloride) is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects. |
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| DC49054 |
ATX inhibitor 8 |
ATX inhibitor 8 is a Autotaxin (ATX) inhibitor extracted from patent WO2018212534A1 compound 96. |
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| DC49125 |
Toddacoumalone |
Toddacoumalone is a natural inhibitor of phosphodiesterase 4 (PDE4) with moderate potency and imperfect drug-like properties. Toddacoumalone has the potential for the research of inflammatory diseases such as psoriasis. |
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| DC49744 |
PDE4-IN-5 |
PDE4-IN-5 (compound 33a) is a potent and selective PDE4 inhibitor (IC50=3.1 nM). PDE4-IN-5 has favorable skin permeability and a well-characterized binding mechanism. Anti-psoriasis effect. |
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| DC49746 |
PF-07038124 |
PF-07038124 is a PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2. PF-07038124 shows inhibitory activities against IL-13, IL4, and IFNγ (IC50=125, 4.1 1.06 nM, respectively). |
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| DC49747 |
PDE4-IN-8 |
PDE4-IN-8 (Example 5) is a potent PDE4 inhibitor with an IC50 of 0.93 nM for PDE4B2.PDE4-IN-8 has little effect on IL13 (IC50=4.04 nM), IL4 (IC50=36.33 nM), IFNy (IC50=2394 nM). |
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| DC70144 |
GSK-256066 |
A potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively; displays >380,000-fold selectivity over PDE1/23/5/6/7; inhibits TNFα production by lLPS-stimulated human peripheral blood monocytes with IC50 of 0.01 nM; inhibites LPS-induced pulmonary neutrophilia with ED50 of 1.1 ug/kg (aqueous suspension) and 2.9 ug/kg (dry powder formulation) in rats. |
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| DC70165 |
AA6216 |
AA6216 (AA 6216) is novel potent, selective PDE4 inhibitor with IC50 of 0.63 nM.AA6216 showed stronger inhibitory effects against PDE4 than other PDE family members. AA6216 potently inhibits cytokine production (TNF-α,IL-12p40, IL-4, and IL-13, IC50s=2.2-7.9 nM) by PBMCs stimulated with PHA.AA6216 inhibited the production of TGF-β1 by a human monocytic cell line THP-1, AA6216 dose-dependently reduced the production of TNF-α by alveolar macrophages from patients with IPF.AA6216 demonstrated anti-fibrotic potency on mouse model of bleomycin-induced lung fibrosis. |
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| DC70239 |
BAY 2666605
Featured
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BAY2666605 is a potent, small molecule PDE3A-SLFN12 complex inducer with EC50 of 7 nM.BAY2666605 triggers the formation of a complex of two proteins called SLFN12 and PDE3A. This complex drive cancer cells into cell death by a mechanism called apoptosis. |
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| DC70277 |
BVQ1814 |
BVQ1814 (BVQ-1814) is a highly effective fluorescent probe targeting PDE10A with highly potent affinity (IC50=0.9 nM), >1000-fold subfamily selectivity. |
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| DC70322 |
CPL500036 |
CPL500036 (CPL-500036) is a highly potent, selective and orally bioavailable PDE10A inhibitor with IC50 of 35 nM.CPL500036 is highly selective for PDE10A over other PDEs and common off-targets.CPL500036 effectively penetrates the brain where increases cAMP/cGMP levels and phosphorylates effector proteins like AMPA subunits.CPL500036 reduced sensorimotor deficits in 6-OHDA-lesioned rats.Acute and chronic CPL500036 did not reduce effects of L-DOPA in sensorimotor tests.Chronic CPL500036 treatment did not decrease L-DOPA-induced contralateral rotation. |
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| DC70576 |
LY2775240 |
LY2775240 (LY-2775240) is a highly selective, potent and orally active inhibitor of phosphodiesterase 4 (PDE4) with IC50 of 0.09/0.09/2.4/0.14 nM for PDE4A/B/C/D.LY2775240 displays >200-fold selectivity over PDE10A, and >5000-fold selectivity over other PDE isoforms (IC50>10 uM).LY2775240 potently inhibits TNFα secreted induced by Toll‐like receptor 4 agonist LPS in a human whole blood assay, inhibited LPS‐stimulated TNFα but has no effect with the media‐only control.LY2775240 is more potent than apremilast (IC50, 18 nM vs. 290 nM), also affects E‐selectin, secreted IgG, plasminogen activator inhibitor‐1, and secreted IL‐10. |
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| DC70683 |
PF-04827736 |
PF-04827736 ((S)-PF-04677490) is a potent, selective PDE1 inhibitor with IC50 of 42, 9.1 and 38 nM for PDE1A, PDE1B and PDE1C, respectively; displays >10-fold selectivity over PDE10A1, and >45-fold selectivity over other PDE isoforms. |
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| DC71151 |
T-0156 |
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway. |
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| DC71384 |
Roflupram |
Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC50 of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors. |
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| DC71385 |
NPD-001 |
NPD-001 is a potent Trypanosoma brucei phosphodiesterases TbrPDEB1 and TbrPDEB2 inhibitor, with IC50 values of 4 and 3 nM, respectively. NPD-001 also inhibits human PDEs (phosphodiesterases). NPD-001 shows good anti trypanosomal activity, with an IC50 of 80 nM. |
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| DC71683 |
Lodenafil
Featured
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Lodenafil (Hydroxyhomosildenafil) is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED). |
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| DC71812 |
Avanafil dibenzenesulfonate |
Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis. |
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| DC72219 |
Ambuphylline |
Ambuphylline (Bufylline) is a bronchodilator. Ambuphylline is a theophylline derivative possibly acting through phosphodiesterase inhibition. Ambuphylline can be used for the research of asthma and other lung diseases. |
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| DC72220 |
(R)-Irsenontrine |
(R)-Irsenontrine ((R)-E2027), the R-enantiomer of Irsenontrine, is a potent phosphodiesterase 9 (PDE9) inhibitor with an IC50 value of 0.041 μM. (R)-Irsenontrine can be used for the research of neurological diseases. |
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| DC72221 |
Phenacaine |
Phenacaine (Holocaine) is a local anesthetic. Phenacaine inhibits the specific calmodulin-dependent stimulation of erythrocyte Ca2+-ATPase and cyclic nucleotide phosphodiesterases from brain and heart. |
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| DC72376 |
PF-03049423 free base |
PF-03049423 (Compound PF-5) free base is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 free base can be used for the research of acute ischaemic stroke. |
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